| 词条 | BNC-210 |
| 释义 |
| IUPAC_name = L-Isoleucyl-L-tryptophan | image = IW-2143_molecular_structure.png | CAS_number = | ATC_prefix = none | ATC_suffix = | PubChem = 7019084 | DrugBank = | ChemSpiderID = 5382052 | C=17 | H=23 | N=3 | O=3 | smiles = CC[C@H](C)[C@@H](C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)O)N | StdInChI = 1S/C17H23N3O3/c1-3-10(2)15(18)16(21)20-14(17(22)23)8-11-9-19-13-7-5-4-6-12(11)13/h4-7,9-10,14-15,19H,3,8,18H2,1-2H3,(H,20,21)(H,22,23)/t10-,14-,15-/m0/s1 | StdInChIKey = BVRPESWOSNFUCJ-LKTVYLICSA-N | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | pregnancy_AU = | pregnancy_US = | pregnancy_category= | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = Investigational | routes_of_administration = }}BNC210 (also known as IW-2143 during its time licensed to Ironwood Pharmaceuticals) is an anxiolytic drug that acts via negative allosteric modulation of the α7-nicotinic acetylcholine receptor,[1] by Bionomics Limited. It is currently being investigated for the treatment of post traumatic stress disorder.[2] The drug has demonstrated clinically significant anxiety reduction in both animal models and in Phase I trials.[3] It appears to be devoid of significant sedation or memory-impairing side effects, as well as lacking addictive potential in rat discriminatory models.[4] Phase I trials have shown no serious side effects. Bionomics previously licensed it to Ironwood Pharmaceuticals in January 2012, where it was known as IW-2143. In December 2012, IW-2143 begun undergoing phase I clinical trials in the United States,[5] but in November 2014, was released back to Bionomics in a mutual agreement.[6] Bionomics will now continue development and clinical testing, with Ironwood receiving a royalty for their work done. As of April 2015, BNC210 is in phase II clinical trials.[7] The estimated study completion date is September of 2018. [8] Study DetailsThe clinical trial is currently testing twice daily oral dosages of 600 mg, 300 mg, and 150 mg, for 12 weeks. [9] The primary objective of the trial is for the treatment of PTSD with a secondary objective for the effectiveness in treating anxiety disorders and depression. [10] See also
References1. ^http://www.bionomics.com.au/upload/investors/asx-announcements/4736/ASX695%20%20BNC210%20Phase%201b%20initiation.pdf {{Anxiolytics}}{{Nicotinic acetylcholine receptor modulators}}{{Tryptamines}}{{anxiolytic-stub}}2. ^{{cite web | url = https://clinicaltrials.gov/ct2/show/NCT02933606 | title = www.clinicaltrials.gov | author = Clinicaltrials.gov | publisher = Clinicaltrials.gov | format = HTML | accessdate = 2018-01-04}} 3. ^{{cite web | title = Bionomics - Pipeline | url = http://www.bionomics.com.au/page.php?section=104 | accessdate = 2010-11-09 | quote = Bionomics has discovered a novel compound, BNC210, that offers dramatic competitive advantages over existing treatments | ref = refPipeline}} 4. ^{{cite web | title = BNC210: A Novel Compound with Potent Anxiolytic Activity | url = http://www.bionomics.com.au/siteFiles/files/news/Announcements_295.pdf | accessdate = 2010-11-09 | author = O'Connor, S. | author2 = Andriambeloson, E. | author3 = Huyard, B. | author4 = Wagner, S. | author5 = Sleebs, B. | author6 = Quasi, N. | author7 = Bui, C. | author8 = Street, I. | format = PDF | publisher = Bionomics Limited | quote = By applying a targeted medicinal chemistry strategy beginning from a compound cited in the literature, Bionomics has developed BNC210 | ref = refOConnor}} 5. ^http://investor.ironwoodpharma.com/releasedetail.cfm?ReleaseID=733540 6. ^http://www.biotechdaily.com.au/media/backissues/2014/11%20Nov/BD%20Biotech%20Daily%20Nov%2011.pdf 7. ^{{cite web | url = http://www.prnewswire.com/news-releases/bionomics-initiates-phase-ii-clinical-trial-of-bnc210-for-treatment-of-anxiety-300068306.html | title = www.prnewswire.com | author = Bionomics Limited | publisher = PRNewswire | format = HTML | accessdate = 2015-06-10}} 8. ^{{cite web | url = https://clinicaltrials.gov/ct2/show/NCT02933606 | title = www.clinicaltrials.gov | author = Clinicaltrials.gov | publisher = Clinicaltrials.gov | format = HTML | accessdate = 2018-01-04}} 9. ^{{cite web | url = https://clinicaltrials.gov/ct2/show/NCT02933606 | title = www.clinicaltrials.gov | author = Clinicaltrials.gov | publisher = Clinicaltrials.gov | format = HTML | accessdate = 2018-01-04}} 10. ^{{cite web | url = https://clinicaltrials.gov/ct2/show/NCT02933606 | title = www.clinicaltrials.gov | author = Clinicaltrials.gov | publisher = Clinicaltrials.gov | format = HTML | accessdate = 2018-01-04}} 4 : dipeptides|Anxiolytics|Nicotinic antagonists|Experimental drugs |
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